DE60126762D1 - Kombinatorische Herstellung von Nukleotid- und Nukleosid- (XITP) Analogen - Google Patents

Kombinatorische Herstellung von Nukleotid- und Nukleosid- (XITP) Analogen

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Publication number
DE60126762D1
DE60126762D1 DE60126762T DE60126762T DE60126762D1 DE 60126762 D1 DE60126762 D1 DE 60126762D1 DE 60126762 T DE60126762 T DE 60126762T DE 60126762 T DE60126762 T DE 60126762T DE 60126762 D1 DE60126762 D1 DE 60126762D1
Authority
DE
Germany
Prior art keywords
compound
nucleic acid
alkyl
formula
nucleoside
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
DE60126762T
Other languages
English (en)
Other versions
DE60126762T2 (de
Inventor
Philippe Marliere
Sylvie Pochet
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Centre National de la Recherche Scientifique CNRS
Institut Pasteur de Lille
Original Assignee
Centre National de la Recherche Scientifique CNRS
Institut Pasteur de Lille
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Centre National de la Recherche Scientifique CNRS, Institut Pasteur de Lille filed Critical Centre National de la Recherche Scientifique CNRS
Application granted granted Critical
Publication of DE60126762D1 publication Critical patent/DE60126762D1/de
Publication of DE60126762T2 publication Critical patent/DE60126762T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/044Pyrrole radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/052Imidazole radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/056Triazole or tetrazole radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/10Processes for the isolation, preparation or purification of DNA or RNA
    • C12N15/102Mutagenizing nucleic acids
    • CCHEMISTRY; METALLURGY
    • C40COMBINATORIAL TECHNOLOGY
    • C40BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00Libraries per se, e.g. arrays, mixtures
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
DE60126762T 2000-06-14 2001-06-13 Kombinatorische Herstellung von Nukleotid- und Nukleosid- (XITP) Analogen Expired - Lifetime DE60126762T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR0007557 2000-06-14
FR0007557A FR2810322B1 (fr) 2000-06-14 2000-06-14 PRODUCTION COMBINATOIRE D'ANALOGUES DE NUCLEOTIDES ET NUCLEOTIDES (XiTP)
PCT/FR2001/001830 WO2001096354A1 (fr) 2000-06-14 2001-06-13 PRODUCTION COMBINATOIRE D'ANALOGUES DE NUCLEOTIDES ET NUCLEOSIDES(XiTP)

Publications (2)

Publication Number Publication Date
DE60126762D1 true DE60126762D1 (de) 2007-04-05
DE60126762T2 DE60126762T2 (de) 2007-11-08

Family

ID=8851237

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60126762T Expired - Lifetime DE60126762T2 (de) 2000-06-14 2001-06-13 Kombinatorische Herstellung von Nukleotid- und Nukleosid- (XITP) Analogen

Country Status (14)

Country Link
US (2) US7319148B2 (de)
EP (2) EP1780214A3 (de)
JP (2) JP4460216B2 (de)
AT (1) ATE354581T1 (de)
AU (2) AU6763801A (de)
CA (1) CA2411036A1 (de)
DE (1) DE60126762T2 (de)
DK (1) DK1290006T3 (de)
ES (1) ES2282266T3 (de)
FR (1) FR2810322B1 (de)
MX (1) MXPA02011896A (de)
NZ (1) NZ523090A (de)
PT (1) PT1290006E (de)
WO (1) WO2001096354A1 (de)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4942915B2 (ja) * 2002-04-26 2012-05-30 ギリアード サイエンシーズ, インコーポレイテッド Hivプロテアーゼ阻害剤化合物のホスホネートアナログの細胞蓄積
WO2004096287A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
EA200501676A1 (ru) 2003-04-25 2006-04-28 Джилид Сайэнс, Инк. Фосфонатсодержащие ингибиторы киназы (варианты), способ их получения, фармацевтическая композиция, лекарственная форма на их основе и способ ингибирования киназы у млекопитающего (варианты)
US7407965B2 (en) 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
WO2004096285A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
ATE490788T1 (de) 2003-04-25 2010-12-15 Gilead Sciences Inc Antivirale phosphonate analoge
WO2005002626A2 (en) 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
US7470724B2 (en) 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
CN100503628C (zh) * 2003-05-30 2009-06-24 法莫赛特股份有限公司 修饰的氟化核苷类似物
US7947817B2 (en) * 2003-06-30 2011-05-24 Roche Molecular Systems, Inc. Synthesis and compositions of 2'-terminator nucleotides
EP1680512A1 (de) 2003-10-24 2006-07-19 Gilead Sciences, Inc. Verfahren und zusammensetzungen zur identifizierung therapeutischer verbindungen
WO2005044308A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
WO2005044279A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
JP2007515495A (ja) 2003-12-22 2007-06-14 ギリアード サイエンシーズ, インコーポレイテッド 4’−置換カルボビル誘導体およびアバカビル誘導体ならびにhivおよびhcv抗ウイルス活性を有する関連化合物
US7745125B2 (en) 2004-06-28 2010-06-29 Roche Molecular Systems, Inc. 2′-terminator related pyrophosphorolysis activated polymerization
CN101023094B (zh) * 2004-07-21 2011-05-18 法莫赛特股份有限公司 烷基取代的2-脱氧-2-氟代-d-呋喃核糖基嘧啶和嘌呤及其衍生物的制备
TR201906416T4 (tr) 2004-07-27 2019-05-21 Gilead Sciences Inc Hiv inhibitörü bileşiklerin fosfonat analogları.
WO2006031725A2 (en) * 2004-09-14 2006-03-23 Pharmasset, Inc. Preparation of 2'­fluoro-2'- alkyl- substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives
EP2061316A4 (de) * 2006-09-11 2011-08-24 Southern Res Inst Azolnukleoside und verwendung als hemmer variabler rna- und dna-polymerasen
US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
PE20110219A1 (es) 2008-07-08 2011-03-31 Gilead Sciences Inc Sales del compuesto n-[(s)({[(2r,5r)-5-(6-amino-9h-purin-9-il)-4-fluoro-2,5-dihidrofuran-2-il]oxi}metil)fenoxifosfinoil]-l-alaninato de etilo como inhibidores de vih
WO2010075549A2 (en) 2008-12-23 2010-07-01 Pharmasset, Inc. Nucleoside phosphoramidates
US8551973B2 (en) 2008-12-23 2013-10-08 Gilead Pharmasset Llc Nucleoside analogs
CN102325783A (zh) 2008-12-23 2012-01-18 法莫赛特股份有限公司 嘌呤核苷的合成
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
TWI576352B (zh) 2009-05-20 2017-04-01 基利法瑪席特有限責任公司 核苷磷醯胺
SI3290428T1 (sl) 2010-03-31 2022-01-31 Gilead Pharmasset Llc Tableta, ki obsega kristalinični (S)-izopropil 2-(((S)-(((2R,3R,4R,5R) -5-(2,4-diokso-3,4-dihidropirimidin-1(2H)-il)-4-fluoro-3-hidroksi-4- metiltetrahidrofuran-2-il)metoksi)(fenoksi)fosforil)amino)propanoat
US8563530B2 (en) 2010-03-31 2013-10-22 Gilead Pharmassel LLC Purine nucleoside phosphoramidate
AR084044A1 (es) 2010-11-30 2013-04-17 Pharmasset Inc Compuestos 2’-espiro-nucleosidos
US8889159B2 (en) 2011-11-29 2014-11-18 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus
SG11201600919UA (en) 2013-08-27 2016-03-30 Gilead Pharmasset Llc Combination formulation of two antiviral compounds
PL3661937T3 (pl) 2017-08-01 2021-12-20 Gilead Sciences, Inc. Formy krystaliczne ((s)-((((2r,5r)-5-(6-amino-9h-puryn-9-ylo)-4-fluoro-2,5-dihydrofuran-2-ylo)oksy)metylo)(fenoksy)fosforylo)-l-alaninianu etylu (gs-9131) do leczenia zakażeń wirusowych

Also Published As

Publication number Publication date
JP2009240321A (ja) 2009-10-22
AU6763801A (en) 2001-12-24
JP2004503559A (ja) 2004-02-05
EP1780214A3 (de) 2008-06-18
EP1780214A2 (de) 2007-05-02
AU2001267638B2 (en) 2006-06-29
MXPA02011896A (es) 2004-09-13
NZ523090A (en) 2005-05-27
ATE354581T1 (de) 2007-03-15
JP4460216B2 (ja) 2010-05-12
DE60126762T2 (de) 2007-11-08
US20040023240A1 (en) 2004-02-05
ES2282266T3 (es) 2007-10-16
FR2810322B1 (fr) 2006-11-10
US20100286386A1 (en) 2010-11-11
DK1290006T3 (da) 2007-06-18
EP1290006B1 (de) 2007-02-21
WO2001096354A1 (fr) 2001-12-20
US7319148B2 (en) 2008-01-15
FR2810322A1 (fr) 2001-12-21
PT1290006E (pt) 2007-05-31
EP1290006A1 (de) 2003-03-12
CA2411036A1 (fr) 2001-12-20

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